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Review
. 2024 Oct 19:19:10623-10637.
doi: 10.2147/IJN.S480095. eCollection 2024.

The Advances in the Development of Epigenetic Modifications Therapeutic Drugs Delivery Systems

Tingyi Li  1   2 , Yanwei Chen  1 , Shuai Li  1
Affiliations
Review

The Advances in the Development of Epigenetic Modifications Therapeutic Drugs Delivery Systems

Tingyi Li et al. Int J Nanomedicine. .

Abstract

Epigenetic dysregulation can significantly trigger the onset and progression of various diseases, epigenetic therapy is a new treatment strategy by changing DNA methylation, histone modification, N6-methyladenosine, chromatin modification and other epigenetic modifications to regulate gene expression levels for therapeutic purposes. However, small-molecule epigenetic drugs face challenges in disease treatment, such as lack of selectivity, limited therapeutic efficacy, and insufficient safety. Nanomedicine delivery systems offer significant advantages in addressing these issues by enhancing drug targeting, improving bioavailability, and reducing nonspecific distribution. This help minimize side effects while increasing both therapeutic effectiveness and safety of epigenetic drugs. In this review, we focus on the mechanism and role of epigenetic regulatory factors in diseases, as well as the challenges faced by small molecule inhibitors in treatment strategies, especially the research advancements in epigenetic drug delivery systems, review and discuss the therapeutic potential and challenges of using nanotechnology to develop epigenetic drug delivery systems.

Keywords: DNA methylation; N6-methyladenosine; epigenetic therapy; histone modification; nanomedicine delivery systems; nanotechnology.

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Conflict of interest statement

The authors declare no conflicts of interest in this work.

Figures

Figure 1
Figure 1
(A) Major processes of DNA methylation and histone modification, including transcriptional repression (B) BRD4 Connection. (C) M6A methylation. M6A methylation is a dynamic and reversible process and the demethylation process is mainly carried out by the FTO and ALKBH5.
Figure 2
Figure 2
Vehicles for transport and delivery of iDNMTs in poly(lactic-co-glycolic acid) (PLGA)- and poly(ethylene glycol) (PEG)-based nanomicelles, in gelatinase with PEG and poly-ε-caprolactone (PCL), and in alendronate-PEG-2-distearoyl-sn-glycero-3-phosphoethanolamine (DSPE).
Figure 3
Figure 3
Illustration depicting experimental drug conditions. PKD1-Het cells were treated with Aza, free MT and Aza (F-MTAza), or MT and Aza delivered within a nanoparticle (NP-MTAza).
Figure 4
Figure 4
(A) Preparation of PGRsEV-siYTHDF1. (B) PGRsEV-siYTHDF1 inhibits gastric cancer progression by targeting FZD7 and modulating its translation through an m6A-dependent mechanism. This action disrupts the Wnt/β-catenin signaling pathway. Additionally, it enhances immunotherapy by promoting the self-presentation of immunogenic tumor antigens and employing a CD47 blockade strategy, which intensifies the cytotoxic effects of cytotoxic T lymphocytes (CTLs) and tumor-associated macrophages (TAMs).
See this image and copyright information in PMC

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